Preparation and evaluation of floating drug delivery system (fdds) containing an antiviral drug
Abstract
Acyclovir, an antiviral drug has low oral bioavailability of about 15-30%. It shows more absorption in the upper gastro intestinal tract. The main objective is to evaluate the potential of floating alginate beads as a drug carrier for acyclovir to prolong gastric residence time of drug in its absorption window. Floating beads were prepared from sodium alginate solution containing CaCO3 as gas-forming agent using Ionotropic gelation method. To overcome the limitation of drug leaching during preparation and to have improved sustained release characteristics, alginate beads were prepared with the addition of polymers like Hydroxy propyl methyl cellulose (HPMC K4M), Eudragit RL 100 and Xanthan gum. Beads were also prepared by using Pectin (polyelectrolyte) containing cross linking solution. The compatibility of drug with the polymer was confirmed through the FT-IR studies. The prepared beads were evaluated for percentage drug loading, entrapment efficiency, surface morphology and in vitro release characteristics to know the effect of addition of these polymers to alginate solution and the addition of Pectin to cross linking solution. Pectin treated beads prepared with Xanthan gum & Pectin not only showed improved percentage drug loading but also exhibited sustained drug release in the pH 1.2. So these floating alginate beads may act as a promising carrier for acyclovir to improve its oral bioavailability.
Downloads
References
2. Ray-Neng C, Hsiu-O H, Chiao-Ya Y, Ming-Thau S, Development of Swelling/floating gastroretentive drug delivery system based on a combination of hydroxylethyl cellulose and sodium carboxymethyl cellulose for Losartan and its clinical relevance in healthy volunteers with CYP2C9 polymorphism. European Journal of Pharmaceutical Sciences 2010 Nov10 (39):82-89.
3. Brahma N. Singh, Kwon H. Kim. Floating drug delivery systems: an approach to oral controlled drug delivery via gastric retention Drug Delivery Systems. Journal of Controlled Release 2000 (63):235-259.
4. Gopalakrishnan S. and Chenthilnathan A. Floating Drug Delivery Systems: A Review India. Journal of Pharmaceutical Science and Technology 2011 3(2):548-554.
5. Eisen, S.A., Miller, D.k., Woodward, R.S., Spitznagel, E., Przybeck, T.R., 199, the effect of prescribed daily dose frequency on patient medication compliance. Arch. Intern. Med. 150, 1881-1884.
6. Getsios, D., Caro, JJ, Ishak, K.J., El-Hadi, W., Payne, K., OConnel, M., Albrecht, D. Feng. W., Dubois, D., 2004. Oxybutynin Extended Release and Tolterodine Immediate Release: A Health Economic Comparison. Clinical Drug Investigation 24, 81-88.
7. Sansom, L.N., 1999, Oral extended release products. Aust. Prescr. 22 88-90.
8. Hoffman, A., 1998. Pharmacodynamic aspects of sustained release preparations. Advanced Drug Delivery Reviews 33, 185-199.
9. Kumar, M.N., Kumar, N., 2001. Polymeric controlled drug-delivery systems: perspective issues and opportunities. Drug Dev. Ind. Pharm. 27, 1-30.
10. Siepmann, J., Siepmann, F., 2008. The Modified-Release Drug Delivery Landscape: Academic Viewpoint, in: Rathbone, M.J., Hadgraft, J., Roberts, M.S., Lane, M.E. (Eds.), Modified release drug delivery technology, Second ed. Informa Healthcare USA, Inc., New York, pp. 17-34.
11. Hoffman, A., Stepensky, D., Lavy, E., Eyal, S., Klausner, E., Friedman, M., 2004. Pharmacokinetic and pharmacodynamic aspects of gastroretentive dosage forms. Int J Pharm 277, 141-153.
12. Davis, S.S., Hardy, J.G., Taylor, M.J., Whalley, D.R., Wilson, C.G., 1984. A comparative study of the gastrointestinal transit of a pellet and tablet formulation. Int. J. Pharm. 21, 167-1 77.
13. Rouge, N., Buri, P., Doelker, E., 1996. Drug absorption sites in the gastrointestinal tract and dosage forms for site-specific delivery. Int. J. Pharm. 136, 117-139
14. Banker GS, Rhodes CT. Modern Pharmaceutics, Marcel Dekker, New York 1996 :3 :125-128.
15. Desai S& Bolton S. A floating controlled release drug delivery system: in vitro- in vivo evaluation. Pharm Res. 1993; 10:1321-1325.
16. Wilson CG & Washington N. The stomach: its role in oral drug delivery. In: Rubinstein MH, ed. Physiological Pharmaceutical: Biological Barriers to Drug Absorption. Chichester, UK: Ellis Horwood. 1989; 47-70.
17. Desai, S. A floating controlled release drug delivery system: in vitro- in vivo evaluation. Pharm Res. 1993: 10(9): 1321-1325.
18. Mathur P.An overview on recent advancements and developments in gastroretentivebuoyant drug delivery system. Pelagia Res Lib Der Pharmacia Sinica. 2011: 2(1): 161-169.
19. Tiwari A. The Floating Drug Delivery System and Its Impact on Calcium Channel Blocker:A Review Article. Int J Pharma Res & Dev. 2012: 12(3): 107 -131.
20. Vedha HB. The Recent Developments on Gastric Floating Drug Delivery Systems; An Overview. Int J Pharm Tech Res. 2010; 1(2): 524-534.
21. Streubel A, Siepmann J, Bodmeier R. Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release. Eur.J. Pharm. Sci. 2003: 18 :37-45.
22. Bettina B. Masoud G, Fengfu L. Controlled release of acyclovir trough bioengineered corneal implants with silica nanoparticles carries. The open Tissue Engineering and Regenerative Medicine Journal. 2010:3:10-17.
23. Remeth JD, Sfurti SS, Kailas KM. Design and development of mucoadhesive acyclovir tablet, Iranian Journal of Pharmaceutical Research. 2009; 8(4):231-239.
24. Chordiya y. Floating drug delivery system a versatile approach for gastric retention IJPFR. 2011; 1(3): 96-1 12.
25. Bardonnet PL, Gastroretentive Dosage Forms: Overview and Special case of Helicobacter pylori. J Control Rel. 2006; 111: 1-18.
26. Babu Vm. In vitro and In vivo studies of sustained release floating dosage forms containing salbutamol sulphate. Pharmazie. 1990; 45: 268-270.
27. Geetha A, Kumar J. Rajendra, Mohan CH. Krishna. Review on: Floating drug delivery systems. International journal of pharmaceutical research and biomedical analysis. 2012: (1): 1-13.
28. Grubel P, et al. Gastric emptying of nondigestible solids in the fasted dog. J PharmSci. 1987; 76: 117-122.
29. Garg S. and Sharma S. Gastroretentive Drug Delivery System, Business Briefing: Pharmatech. 2003; 7: 160-166.
30. Vyas SP, Khar RK. Gastroretentive systems, In: Controlled drug Delivery. VallabhPrakashan. Delhi, India. 2006; 197-217.
31. Clarke GM, Newton JM, Short MD. Gastrointestinal transit of pellets of differing size and density. Int J Pharm 1993; 100(13): 81-92.
32. Sungthongjeen S, Paeratakul 0, Limmatvapirat S, Puttipupathachorn S. Preparation and in-vitro evaluation of multiple-unit floating drug delivery system based on gas formation technique. Int J Pharm 2006: 324: 136-43.

This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Copyright © Author(s) retain the copyright of this article.